奈莫柔比星

生物活性体外研究体内研究奈莫柔比星试剂级价格

奈莫柔比星

CAS号:108852-90-0
英文名:Nemorubicin
中文名:奈莫柔比星
CBNumber:CB11179292
分子式:C32H37NO13
分子量:643.64
MOL File:108852-90-0.mol

奈莫柔比星化学性质

沸点 :852.2±65.0 °C(Predicted)
密度 :1.55±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO:60.0(Max Conc. mg/mL);101.0(Max Conc. mM)
酸度系数(pKa) :7.35±0.60(Predicted)
形态 :Powder
颜色 :Orange to reddish brown

奈莫柔比星性质、用途与生产工艺

生物活性 Nemorubicin (Methoxymorpholinyl doxorubicin) 是一种具有有效抗肿瘤活性的 Doxorubicin 衍生物。Nemorubicin 对多药耐药表型的多种肿瘤细胞系具有细胞毒性。Nemorubicin 需要完整的核苷酸切除修复系统才能发挥其活性。
体外研究

Nemorubicin has antitumor activity, with IC ₇₀ s of 578 nM, 468 nM, 193 nM, 191 nM, 68 nM, and 131 ± 9 nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cell lines, respectively.
Nemorubicin is CYP3A-activated anticancer prodrug, which can produce a more cytotoxic metabolite, PNU-159682.
Nemorubicin acts through nucleotide excision repair (NER) system to exert its activity. Nemorubicin (0-0.3 μM) is more active in the L1210/DDP cells with intact NER than in the XPG-deficient L1210/0 cells. Cells resistant to nemorubicin show increased sensitivity to UV damage.
Nemorubicin is cytotoxic to 9L/3A4 cells, with an IC ₅₀ of 0.2 nM, 120-fold lower than that of P450-deficient 9L cells (IC ₅₀ , 23.9 nM). Nemorubicin also potently inhibits Adeno-3A4 infected U251 cells with IC ₅₀ of 1.4 nM. P450 reductase overexpression enhances cytotoxicity of Nemorubicin.
体内研究

Nemorubicin is converted to PNU-159682 by human liver cytochrome P450 (CYP) 3A4 in rat, mouse, and dog liver microsomes. Nemorubicin (60 µg/kg) induces sifnificant tumor growth delay in scid mice bearing 9L/3A4 tumors, but shows no obvious effect on the tumor growth delay of 9L tumors in mice by i.v. or intratumoral injection (i.t.). Nemorubicin (40 µg/kg, i.p.) exhibits no antitumor activity and no host toxicity in mice bearing 9L/3A4 tumors.